Polyion complex micelles of core-shell structure

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/34 (2006.01) A61K 9/51 (2006.01) A61K 48/00 (2006.01) B01J 13/00 (2006.01) C08G 69/10 (2006.01) C08G 69/40 (2006.01) C08J 3/02 (2006.01) C12N 15/88 (2006.01) A61K 9/107 (2006.01)

Patent

CA 2391964

A method of stabilizing polyion complex micelles of a core/shell structure comprising a polyelectrolyte and a block copolymer comprising a hydrophilic segment and a chargeable segment. The stabilization method is accomplished by fixing at least one thiol residue to the core-forming chargeable segment of each of block copolymer molecules to thereby form, between these chargeable segments, stable disulfide bond crosslinks through the thiol residues fixed thereto. Representative examples of the copolymer capable of being prepared by the stabilization method include ones represented by general formulae (I), (II), and (III). Thus, a method for stabilizing polyion complex micelles utilizable as a carrier for polyelectrolytes can be provided.

L'invention porte sur un procédé de stabilisation de micelles de complexe de polyions de structure noyau/coque comportant un polyélectrolyte et un copolymère bloc comprenant un segment hydrophile et un segment chargeable. Le procédé de stabilisation consiste à fixer au moins un groupe thiol au segment chargeable formant le noyau de chacune des molécules du polymère bloc de manière à former entre les segments chargeables des liaisons réticulées stables de bisulfure par l'intermédiaire des groupes thiol leur étant fixés. Des exemples représentatifs de copolymères pouvant se préparer à l'aide dudit procédé sont illustrés par les formules générales (I), (II) et (III). Il s'agit donc d'un procédé de stabilisation de micelles de complexe de polyions utilisables comme supports de polyélectrolytes.

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